Antiproliferative and cytotoxic activity of Geraniaceae plant extracts against five tumor cell lines

Aim: To determine the antiproliferative and cytotoxic activities of Geranium and Erodium species against human cancer and noncancer cell lines, respectively. Methods: Twenty-one species of Geranium and Erodium were extracted and screened against cancerous and noncancerous human cell lines. Results: In a dose-response manner, G. glaberrimum, G. asphodeloides, E. brandianum and E. leucanthum were able, with variable potency, to inhibit cellular proliferation. Except for E. brandianum, all extracts induced cellular autophagy in tumor cells with similar levels to that of rapamycin; but, only E. brandianum induced cellular apoptosis, likely through Bcl2 and BAX protein expressions. Discussion: This is the first study to report the potential antiproliferative effects of ethanol extracts of several Geraniaceae species.

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Synthesis of Icaritin and β-anhydroicaritin Mannich Base Derivatives and Their Cytotoxic Activities on Three Human Cancer Cell Lines

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520616666160404111210 ◽

2016 ◽

Vol 17 (1) ◽

pp. 137-142 ◽

Cited By ~ 11

Author(s):

Van-Son Nguyen ◽

Ling Shi ◽

Sheng-Chun Wang ◽

Qiu-An Wang

Keyword(s):

Cell Lines ◽

Cancer Cell ◽

Mannich Base ◽

Human Cancer ◽

Cancer Cell Lines ◽

Cytotoxic Activities ◽

Human Cancer Cell ◽

Human Cancer Cell Lines

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ent-Kaurane Diterpenes from Annona glabra and Their Cytotoxic Activities

Natural Product Communications ◽

10.1177/1934578x1400901204 ◽

2014 ◽

Vol 9 (12) ◽

pp. 1934578X1400901

Author(s):

Hoang Le Tuan Anh ◽

Nguyen Thi Thu Hien ◽

Dan Thi Thuy Hang ◽

Tran Minh Ha ◽

Nguyen Xuan Nhiem ◽

...

Keyword(s):

Cell Lines ◽

Cancer Cell ◽

Human Cancer ◽

2D Nmr ◽

Cancer Cell Lines ◽

Cytotoxic Activities ◽

Human Cancer Cell ◽

2D Nmr Spectroscopy ◽

Human Cancer Cell Lines ◽

Annona Glabra

A new ent-kaurane glycoside, annoglabasin H (1), and three known ent-kauranes, annoglabasin E (2), annoglabasin B (3), and 19-nor- ent-kaurent-4-ol-17-oic acid (4) were isolated from the fruits of Annona glabra. Their structures were determined by the combination of spectroscopic and chemical methods, including 1D- and 2D-NMR spectroscopy, as well as by comparison with the NMR data reported in the literature. The cytotoxic activities of these compounds were evaluated on four human cancer cell lines, LU-1, MCF-7, SK-Mel2, and KB. Compound 1 exhibited significant cytotoxic activity on all tested human cancer cell lines with IC50 values ranging from 3.7 to 4.6 μM.

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Synthesis, Cytotoxic Activity, Crystal Structure, DFT Studies and Molecular Docking of 3-Amino-1-(2,5-dichlorophenyl)-8-methoxy-1H-benzo[f]chromene-2-carbonitrile

Crystals ◽

10.3390/cryst11020184 ◽

2021 ◽

Vol 11 (2) ◽

pp. 184

Author(s):

Menna El Gaafary ◽

Tatiana Syrovets ◽

Hany M. Mohamed ◽

Ahmed A. Elhenawy ◽

Ahmed M. El-Agrody ◽

...

Keyword(s):

Cytotoxic Activity ◽

Cell Lines ◽

Cancer Cell ◽

Dna Methyltransferase ◽

Human Cancer ◽

Theoretical Calculations ◽

Cancer Cell Lines ◽

Molecular Structures ◽

Cytotoxic Activities ◽

X Ray

The target compound 3-amino-1-(2,5-d ichlorophenyl)-8-methoxy-1H-benzo[f]-chromene-2-carbonitrile (4) was synthesized via a reaction of 6-methoxynaphthalen-2-ol (1), 2,5-dichlorobenzaldehyde (2), and malononitrile (3) in ethanolic piperidine solution under microwave irradiation. The newly synthesized β-enaminonitrile was characterized by FT-IR, 1H NMR, 13C NMR, mass spectroscopy, elemental analysis and X-ray diffraction data. Its cytotoxic activity was evaluated against three different human cancer cell lines MDA-MB-231, A549, and MIA PaCa-2 in comparison to the positive controls etoposide and camptothecin employing the XTT cell viability assay. The analysis of the Hirshfeld surface was utilized to visualize the reliability of the crystal package. The obtained results confirmed that the tested molecule revealed promising cytotoxic activities against the three cancer cell lines. Furthermore, theoretical calculations (DFT) were carried out with the Becke3-Lee-Yang-parr (B3LYP) level using 6-311++G(d,p) basis. The optimization geometry for molecular structures was in agreement with the X-ray structure data. The HOMO-LUMO energy gap of the studied system was discussed. The intermolecular-interactions were studied through analysis of the topological-electron-density(r) using the QTAIM and NCI methods. The novel compound exhibited favorable ADMET properties and its molecular modeling analysis showed strong interaction with DNA methyltransferase 1.

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IL6 sensitizes prostate cancer to the antiproliferative effect of IFNα2 through IRF9

Endocrine Related Cancer ◽

10.1530/erc-13-0222 ◽

2013 ◽

Vol 20 (5) ◽

pp. 677-689 ◽

Cited By ~ 11

Author(s):

Holger H H Erb ◽

Regina V Langlechner ◽

Patrizia L Moser ◽

Florian Handle ◽

Tineke Casneuf ◽

...

Keyword(s):

Prostate Cancer ◽

Cell Lines ◽

Cellular Proliferation ◽

Tissue Expression ◽

Type I ◽

Regulatory Factor ◽

Quantitative Real Time Pcr ◽

Antiproliferative Effects ◽

Protein Levels

Development and progression of prostate cancer (PCa) are associated with chronic inflammation. The cytokine interleukin 6 (IL6) can influence progression, differentiation, survival, and angiogenesis of PCa. To identify novel pathways that are triggered by IL6, we performed a gene expression profiling of two PCa cell lines, LNCaP and MDA PCa 2b, treated with 5 ng/ml IL6. Interferon (IFN) regulatory factor 9 (IRF9) was identified as one of the most prevalent IL6-regulated genes in both cell lines. IRF9 is a mediator of type I IFN signaling and acts together with STAT1 and 2 to activate transcription of IFN-responsive genes. The IL6 regulation of IRF9 was confirmed at mRNA and protein levels by quantitative real-time PCR and western blot respectively in both cell lines and could be blocked by the anti-IL6 antibody Siltuximab. Three PCa cell lines, PC3, Du-145, and LNCaP-IL6+, with an autocrine IL6 loop displayed high expression of IRF9. A tissue microarray with 36 PCa tissues showed that IRF9 protein expression is moderately elevated in malignant areas and positively correlates with the tissue expression of IL6. Downregulation and overexpression of IRF9 provided evidence for an IFN-independent role of IRF9 in cellular proliferation of different PCa cell lines. Furthermore, expression of IRF9 was essential to mediate the antiproliferative effects of IFNα2. We concluded that IL6 is an inducer of IRF9 expression in PCa and a sensitizer for the antiproliferative effects of IFNα2.

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Six New neo-Clerodane Diterpenoids from Aerial Parts of Scutellaria barbata and Their Cytotoxic Activities

Planta Medica ◽

10.1055/a-0638-8255 ◽

2018 ◽

Vol 84 (17) ◽

pp. 1292-1299 ◽

Cited By ~ 9

Author(s):

Guo-Chun Yang ◽

Jia-Hui Hu ◽

Bing-Long Li ◽

Huan Liu ◽

Jia-Yue Wang ◽

...

Keyword(s):

Cell Lines ◽

Human Cancer ◽

In Vitro Cytotoxicity ◽

Cytotoxic Activities ◽

Scutellaria Barbata ◽

Human Cancer Cell Lines ◽

Aerial Parts ◽

Ic50 Values ◽

Clerodane Diterpenoids

AbstractSix new neo-clerodane diterpenoids (1–6), scutebatas X – Z, A1-C1, along with twelve known ones (7–18) were obtained via the phytochemical investigation of the aerial parts of Scutellaria barbata. Their structures were established by detailed spectroscopic analysis. The absolute configurations of 1 and 2, as the representative members of this type, were identified based on a circular dichroic exciton chirality method. Moreover, in vitro cytotoxicity of compounds 1–6 were evaluated against three human cancer cell lines (SGC-7901, MCF-7, and A-549) using the MTT method. Compound 6 showed cytotoxic activities against all the three cell lines with IC50 values of 17.9, 29.9, and 35.7 µM, respectively.

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Cytotoxic Sterols from Philippine Mushrooms

Asian Journal of Chemistry ◽

10.14233/ajchem.2020.22591 ◽

2020 ◽

Vol 32 (5) ◽

pp. 1197-1202

Author(s):

Consolacion Y. Ragasa ◽

Glenn G. Oyong ◽

Maria Carmen S. Tan ◽

Mariquit M. De Los Reyes ◽

Maria Ellenita G. De Castro

Keyword(s):

Cell Lines ◽

Cancer Cell ◽

Human Cancer ◽

Dermal Fibroblast ◽

Cancer Cell Lines ◽

Cytotoxic Activities ◽

Cell Viability Assay ◽

Ic50 Values ◽

Ht 29 ◽

Mcf 7

Ergosterol peroxide (1) and ergosterol (2) were commonly isolated as the major compounds of Philippine mushrooms. Sterols 1 and 2 from the dichloromethane extract of Geastrum triplex and Termitomyces clypeatus, respectively, were evaluated for their cytotoxic activities against four human cancer cell lines, viz., breast cancer (MCF-7), colon cancer (HT-29), leukemia (THP-1), and small lung cell carcinoma (H69PR), and a human normal cell line, human dermal fibroblast-neonatal (HDFn), using the PrestoBlue® cell viability assay. Compounds 1 and 2 exhibited the strongest activities against HT-29 with IC50 values of 1.79 and 2.98 μg/mL, respectively, while Zeocin gave an IC50 of 4.89 μg/mL. These compounds also exhibited strong antiproliferative effects against MCF-7 with IC50 values of 4.13 for 1 and 4.20 μg/mL for compound 2, comparable to Zeocin with IC50 = 3.68 μg/mL. Only moderate cytotoxicity resulted when compounds 1 and 2 were tested against H69PR with IC50 values of 7.78 and 6.83 μg/mL, respectively, while Zeocin exhibited an IC50 of 9.81 μg/mL. Furthermore, compounds 1 and 2 showed no effects against THP-1 (IC50 > 100 μg/mL), while Zeocin showed an IC50 of 4.73 μg/mL. Although compounds 1 and 2 have been reported to exhibit different bioactivities in previous studies, the cancer cell lines tested and/or the polarities of the solvents for extraction varied. Therefore, comparisons of the cytotoxic activities of compounds 1 and 2 with earlier studies could not be made extensively.

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Cytotoxic Activities of Different Iranian Solanaceae and Lamiaceae Plants and Bioassay-Guided Study of an Active Extract from Salvia lachnocalyx

Natural Product Communications ◽

10.1177/1934578x1701201009 ◽

2017 ◽

Vol 12 (10) ◽

pp. 1934578X1701201 ◽

Cited By ~ 2

Author(s):

Hossein H. Mirzaei ◽

Omidreza Firuzi ◽

Ian T. Baldwin ◽

Amir Reza Jassbi

Keyword(s):

Cell Lines ◽

Cancer Cell ◽

Human Cancer ◽

Cancer Cell Lines ◽

Active Species ◽

Cytotoxic Activities ◽

Human Cancer Cell ◽

Human Cancer Cell Lines ◽

Bioassay Guided Fractionation ◽

Cytotoxic Compounds

Methanol (MeOH), dichloromethane (DCM) and 80% MeOH extractions of fourteen medicinal plants of the families Solanaceae and Lamiaceae collected from different area of Iran were tested for their cytotoxic potential against MOLT-4 human cancer cell lines. Cytotoxicity of the tested plants indicated that 11 plants had one or two active extracts (IC50 ≤50): MeOH extracts of the shoots of Thymus trautvetteri, Solanum luteum and stems of Lycium shawii; DCM extracts of the shoots of Thymus kotschyanus, Salvia persepolitana, Ballota aucheri, Nepeta glomerulosa, Hyoscyamus tenuicaulis, Salvia lachnocalyx, Salvia sharifii as well as the stems of Salvia verticillata and the roots of Salvia multicaulis and S. lachnocalyx; 80% MeOH extracts of the shoots of T. trautvetteri, S. luteum and the stems of L. shawii. The DCM extract of the aerial parts of S. lachnocalyx as one of the most active species was subjected to the cytotoxic bioassay-guided fractionation and purification using combination of chromatography methods. The bioassay-guided fractionation of DCM extract of the shoots of S. lachnocalyx led to the isolation of two cytotoxic compounds: (2 Z,6 Z,10 Z,14 E)-geranylfarnesol (1), a novel natural product, and spathulenol (2). Both of the isolated compounds, especially 1 (IC50 range: 9.6 −20.2 μg/mL), showed good cytotoxic effects against 3 human cancer cell lines, MOLT-4, MCF-7 and HT-29.

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